30512-65-3Relevant academic research and scientific papers
Design, synthesis, antifungal activity and molecular docking of thiochroman-4-one derivatives
Zhong, Yifan,Han, Xiaoyan,Li, Shengbin,Qi, Hui,Song, Yali,Qiao, Xiaoqiang
, p. 904 - 910 (2017)
N-Myristoyltransferase (NMT) has been validated pre-clinically as a target for treatment of fungal infections. Various substituted thiochroman-4-one derivatives have been synthesized by an efficient method. The synthesized compounds 7a–y and 8a–t were evaluated for their in vitro antifungal activity against the Canidia albicans, Cryptococcus neoformans, Epidermophyton floccosum, Mucor racemosus, Microsporum gypseum and Aspergillus nigerstrain. A series of compounds exhibited significant activity (minimal inhibitory concentrotion (MIC)=0.5–16μg/mL) against Canidia albicans and Cryptococcus neoformans. The antifungal activity of compound 7b was reached to that of fluconazole, which can serve as a good starting point for further studies of structural diversity of the NMT inhibitors. The molecular docking studies revealed an interesting binding profile with very high receptor affinity for NMT of Canidia albicans.
Thiochromanone derivative and preparation method and application thereof
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Paragraph 0042-0044, (2017/07/19)
The invention discloses a thiochromanone derivative and meanwhile discloses a thiochromanone derivative and a preparation method and application thereof. Experimental results show that the compound has the advantages of being wide in antibacterial spectrum, high in selectivity and free of drug resistance, the antibacterial activity level of the derivative is higher, the thiochromanone contained in the derivative has high lipid solubility, the problem that at present, the cytomembrane penetrating power of an NMT inhibitor is insufficient can be improved, and the thiochromanone derivative is used for preparing antibacterial pharmaceutic preparations for treating fungal diseases caused by pathogenic bacteria such as candida albicans, cryptococcus neoformans, aspergillus niger, mucor, microsporum gypseum and epidermophyton floccosum and has huge potential economic benefit and social value.
TRICYCLIC PYRAZOL AMINE DERIVATIVES
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Page/Page column 124, (2011/06/16)
This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
Synthesis and preliminary in vitro biological evaluation of 4-[(4-hydroxyphenyl)sulfanyl]but-3-en-2-one, a 4-mercaptophenol derivative designed as a novel bifunctional antimelanoma agent
Ruzza, Paolo,Rosato, Antonio,Nassi, Alberto,Rondina, Maria,Zorzin, Matteo,Rossi, Carlo Riccardo,Floreani, Maura,Quintieri, Luigi
experimental part, p. 4973 - 4976 (2010/03/02)
We report the synthesis and preliminary in vitro biological evaluations of 4-[(4-hydroxyphenyl) sulfanyl]but-3-en-2-one, a compound designed as a potential bifunctional antimelanoma agent, bearing both a tyrosinase-activatable phenolic moiety and a GSH-re
